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United States Patent | 6,262,094 |
Hoefle ,   et al. | July 17, 2001 |
The invention is concerned with epothilones in which the thiazole substituent has been modified, with methods for their preparation and with antifungal or therapeutic agents which contain these epothilones.
Inventors: | Hoefle; Gerhard (Braunschweig, DE); Glaser; Nicole (Braunschweig, DE); Leibold; Thomas (Wolfenbuttel, DE); Vite; Gregory (Titusville, NJ); Kim; Soong-Hoon (Lawrenceville, NJ) |
Assignee: | Bristol-Myers Squibb Company (Princeton, NJ) |
Appl. No.: | 506481 |
Filed: | February 17, 2000 |
Feb 22, 1999[DE] | 199 07 588 | |
Jul 01, 1999[DE] | 199 30 111 |
Current U.S. Class: | 514/365; 548/204 |
Intern'l Class: | C07D 417/06; A61K 031/425 |
Field of Search: | 548/204 514/365 |
Foreign Patent Documents | |||
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IC.sub.50 [ng/mL] PC-3 SK- L929 KB-3.1 KB-V1* pros- OV-3 A-549 K-562/U-937 Compound mouse cervix cervix tate ovary lung leukemia 21- 170 60 8 10 12 (K- chloro- 562) epo A [3] epo A-20- 7 carb- aldoxime [22a] epo A-20- 12 carb- aldehyde hydrazone 21-azido- 6 epo A [22b] 21-amino- 8 4 30 3 4 3 (U- epo A [9] 937) 20-vinyl- 3 3 3 0.4 1 1.5 (U- epo A 937) [15] 21-azido- 0.6 0.5 0.5 0.4 epo B [7] 21-amino- 0.5 0.4 1.5 1.5 epo B [9] *Multiresistant cell line